2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. Mutant IDH1 inhibitor

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

For research use only. We do not sell to patients.

Mutant IDH1 inhibitor Chemical Structure

Mutant IDH1 inhibitor Chemical Structure

CAS No. : 1429180-08-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 175 In-stock
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10 mg USD 280 In-stock
50 mg USD 690 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Mutant IDH1 inhibitor Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Mutant IDH1 inhibitor

WB

    Mutant IDH1 inhibitor purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758.  [Abstract]

    Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.

    View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

    View All Isoforms
    IDH1 IDH2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

    IC50 & Target

    IC50: < 72 nM (mutant IDH1 R132H)
    In Vitro

    Mutant IDH1 inhibitor is a potent IDH1 R132H inhibitor, and used for the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Mutant IDH1 inhibitor Related Antibodies
    Molecular Weight

    466.58

    Formula

    C25H34N6O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CC(C)[C@@H](COC1=O)N1C2=NC(N[C@@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 34 mg/mL (72.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1433 mL 10.7163 mL 21.4326 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References
    Cell Assay
    [1]

    Day 1: cells are seeded in 384-well plates in triplicates for both the cell proliferation and 2HG assay, and incubated at 37°C, 95% Rh, 5% CO2 overnight. Day 2: compounds are serially diluted 1 :3 (10 point dilution from 10 mM solutions in DMSO) and delivered to the cell assay plates via acoustic dispenser, with final concentration ranging from 30 μM to 1.5 nM. The plates are returned to the incubator after treatment and incubated for 48 hours. Day 4 Proliferation assay: CTG is added to the assay plates and luminescence signal is read on the plate reader. Day 4 2HG assay : Extraction sample preparation consisted of aspirating all media from the assay plates, adding 70 μL of 90% methanol in water, dry ice incubation for 15 minutes, centrifuging at 2000 rpm for 30 min to ensure all particulates have settled, and transferring 30 μL of the supernatant into LC-MS ready plates. LC-MS analysis follows.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1433 mL 10.7163 mL 21.4326 mL 53.5814 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL 10.7163 mL
    10 mM 0.2143 mL 1.0716 mL 2.1433 mL 5.3581 mL
    15 mM 0.1429 mL 0.7144 mL 1.4288 mL 3.5721 mL
    20 mM 0.1072 mL 0.5358 mL 1.0716 mL 2.6791 mL
    25 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
    30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7860 mL
    40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3395 mL
    50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0716 mL
    60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
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    Mutant IDH1 inhibitor Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Mutant IDH1 inhibitor1429180-08-4Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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